Molecular Design, Synthesis, Characterization and Biological Evaluation of 1-Substituted Tetrahydropyrimidine Derivatives by Leuckart Reaction.

Medicinal chemistry is interdisciplinary subject involving organic chemistry, Inorganic chemistry, Biochemistry, Physiology, Microbiology, Biology, Toxicology and Computer modeling in the research for better and new drug discovery. Generally medicinal chemistry is used to make new compound, determine its biological efficacy and alter the structure of the compound for optimum effect. 142 Preliminary screening of the 1-substituted tetrahydropyrimidine derivatives was done by using molinspiration, chemdoodle and chemsketch software. The present study describes the synthesis of 1-substituted tetrahydropyrimidine derivatives by Leuckart reaction. This methodology offers the spirited advantages having lesser time reaction and yield higher percentage of products. Melting point was found for the synthesized compound and purity of the synthesized compound was analyzed by TLC. The structures of the synthesized compounds were elucidated by IR, NMR and Mass spectroscopy. The synthesized compounds were screened for anti oxidant, anticancer, antibacterial, antifungal activity. The in-vitro anti oxidant property for all the compounds showed positive results. The compounds D – E2, D – E3, D – E4, D – E7, D – E8, D – E9 showed more potent activity. These six compounds were selected and evaluated for anticancer activity. The results obtained showed that synthesized compounds D – E3, D – E8, showed anticancer activity against cancer cells. It proves the suitable structural modification will have to be carried to get novel compound having potent anticancer activity with least effect on normal cells. The antimicrobial activities of synthesized compounds were to obtained zone of inhibition by disc diffusion method